Literature DB >> 16297626

Hit-to-Lead studies: the discovery of potent, orally bioavailable thiazolopyrimidine CXCR2 receptor antagonists.

Andrew Baxter1, Anne Cooper, Elizabeth Kinchin, Kerry Moakes, John Unitt, Alan Wallace.   

Abstract

A Hit-to-Lead optimisation programme was carried out on a high throughput screening hit, the thiazolopyrimidine 1, resulting in the discovery of the potent, orally bioavailable CXCR2 antagonist 29.

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Year:  2005        PMID: 16297626     DOI: 10.1016/j.bmcl.2005.10.091

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  5 in total

1.  A rapid access to novel and diverse 3-oxothiazolo[3,2-c]pyrimidine-8-carboxylates using multicomponent Mannich cyclisation reactions.

Authors:  Muhammet Yıldırım; Derya Çelikel
Journal:  Mol Divers       Date:  2014-08-24       Impact factor: 2.943

2.  Targeting lung inflammation: novel therapies for the treatment of COPD.

Authors:  Hongwei Yao; Willem I de Boer; Irfan Rahman
Journal:  Curr Respir Med Rev       Date:  2008

Review 3.  Role of the CXCL8-CXCR1/2 Axis in Cancer and Inflammatory Diseases.

Authors:  Helen Ha; Bikash Debnath; Nouri Neamati
Journal:  Theranostics       Date:  2017-04-07       Impact factor: 11.556

4.  Promising Antidiabetic and Antimicrobial Agents Based on Fused Pyrimidine Derivatives: Molecular Modeling and Biological Evaluation with Histopathological Effect.

Authors:  Fatma Bassyouni; Mohammad Tarek; Abeer Salama; Bassant Ibrahim; Sawsan Salah El Dine; Nemat Yassin; Amina Hassanein; Maysa Moharam; Mohamed Abdel-Rehim
Journal:  Molecules       Date:  2021-04-19       Impact factor: 4.411

Review 5.  Future therapeutic treatment of COPD: struggle between oxidants and cytokines.

Authors:  Willem I de Boer; Hongwei Yao; Irfan Rahman
Journal:  Int J Chron Obstruct Pulmon Dis       Date:  2007
  5 in total

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